申请人:Max-Planck-Gesellschaft zur Förderung der
Wissenschaften e.V.
公开号:EP2993171A1
公开(公告)日:2016-03-09
Novel efficient, time-saving and reliable radiofluorination procedures for the production of 18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with 18F- are described. The active ester including [18F]F-Py-TFP and [18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.
本文描述了一种高效、省时和可靠的放射性氟化程序,通过将相应的离子前体与18F进行亲核取代,制备18F标记的活性酯。其中包括通过这些方法制备的[18F]F-Py-TFP和[18F]TFB等活性酯,用于制备PSMA特异性PET示踪剂,如[18F]DCFPyL。这些创新方法的关键优势是效率高、制备时间短和易于自动化。含有至少一种通过创新方法制备的PSMA特异性PET示踪剂的制药组合物,对于正电子发射断层扫描(PET)成像特别是前列腺肿瘤成像非常有用。